Thursday, October 3, 2013
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Protein phosphatase 2 (PPP2CA; PP2A)
Studies in patient samples
and mice suggest Gilenya fingolimod and
nonimmunosuppressive derivatives could help eradicate leukemic stem cells in
CML, which are associated with disease relapse. In leukemic hematopoietic
stem cells (HSCs) isolated from patients with CML, PP2A activity was lower
than that in healthy HSCs. In the CML stem cells, Gilenya or any of three
nonimmunosuppressive derivatives activated PP2A, impaired self-renewal and
induced apoptosis. In mouse xenograft models of CML, Gilenya decreased
leukemic stem cell numbers compared with no treatment. Next steps include
designing additional PP2A activators.
Novartis AG markets the sphingosine 1-phosphate receptor
agonist Gilenya to treat relapsing forms of multiple sclerosis (MS).
Oncotide Pharmaceuticals Inc.
has SET nuclear oncogene (SET)
inhibitors in preclinical development to treat various cancers. SET
inhibition is designed to activate PP2A.
Published online Oct. 3, 2013
Multiple patent applications
filed covering nonimmunosuppressive derivatives and their use in various cancers;
available for licensing and partnering from The Ohio State
Technology Commercialization and Knowledge Transfer Office
Neviani, P. et al. J.
Clin. Invest.; published online Sept. 3, 2013;
Contact: Danilo Perrotti, University of Maryland, College
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